BR112014011064A8 - 2-oxo-oxazolidin-3,5-diyl antibiotic derivatives - Google Patents

2-oxo-oxazolidin-3,5-diyl antibiotic derivatives

Info

Publication number
BR112014011064A8
BR112014011064A8 BR112014011064A BR112014011064A BR112014011064A8 BR 112014011064 A8 BR112014011064 A8 BR 112014011064A8 BR 112014011064 A BR112014011064 A BR 112014011064A BR 112014011064 A BR112014011064 A BR 112014011064A BR 112014011064 A8 BR112014011064 A8 BR 112014011064A8
Authority
BR
Brazil
Prior art keywords
oxazolidin
oxo
diyl
antibiotic derivatives
alkyl
Prior art date
Application number
BR112014011064A
Other languages
Portuguese (pt)
Other versions
BR112014011064A2 (en
Inventor
Hubschwerlen Christian
Rueedi Georg
Surivet Jean-Philippe
Zumbrunn Acklin Cornelia
Original Assignee
Actelion Pharmaceuticals Ltd
Idorsia Pharmaceuticals Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Actelion Pharmaceuticals Ltd, Idorsia Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of BR112014011064A2 publication Critical patent/BR112014011064A2/en
Publication of BR112014011064A8 publication Critical patent/BR112014011064A8/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Detergent Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

DERIVADOS DE ANTIBIÓTICOS 2-OXO-OXAZOLIDIN-3,5-DIILA. A invenção refere-se aos compostos anti-bacterianos da fórmula I em que R1a representa H ou carboxi e R1b representa H, ou R1a e R1b representam em conjunto seja o grupo *-C (O) -NH-S-# ou o grupo *-C (OH) =N-S-# em que "*" representa o ponto de ligação de R1a e "#" representa o ponto de ligação de R1b; R2 representa H, alquila(C1-C3), hidroxi-alquila(C1-C3), benzila ou cicloalquila(C3-C5); R3 representa H ou halogênio; U representa N ou CR4; em que R4 é H ou alcoxi(C1-C3); A representa CH, B representa NH e m representa 1 ou 2 e n representa 1 ou 2; ou A representa N, B está ausente, m representa 2 e n representa 2; Y representa CH ou N; e Q representa O ou S; e os sais de tais compostos.ANTIBIOTIC DERIVATIVES 2-OXO-OXAZOLIDIN-3,5-DIYLA. The invention relates to antibacterial compounds of the formula I in which R1a represents H or carboxy and R1b represents H, or R1a and R1b together represent either the group *-C(O)-NH-S-# or the group *-C(OH)=N-S-# where "*" represents the attachment point of R1a and "#" represents the attachment point of R1b; R2 represents H, (C1-C3)alkyl, hydroxy(C1-C3)alkyl, benzyl or (C3-C5)cycloalkyl; R3 represents H or halogen; U represents N or CR4; wherein R4 is H or (C1-C3)alkoxy; A represents CH, B represents NH and m represents 1 or 2 and n represents 1 or 2; or A represents N, B is absent, m represents 2 and n represents 2; Y represents CH or N; and Q represents O or S; and the salts of such compounds.

BR112014011064A 2011-11-08 2012-11-07 2-oxo-oxazolidin-3,5-diyl antibiotic derivatives BR112014011064A8 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IB2011054968 2011-11-08
PCT/IB2012/056236 WO2013068948A1 (en) 2011-11-08 2012-11-07 2-oxo-oxazolidin-3,5-diyl antibiotic derivatives

Publications (2)

Publication Number Publication Date
BR112014011064A2 BR112014011064A2 (en) 2017-06-13
BR112014011064A8 true BR112014011064A8 (en) 2017-12-26

Family

ID=47258051

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112014011064A BR112014011064A8 (en) 2011-11-08 2012-11-07 2-oxo-oxazolidin-3,5-diyl antibiotic derivatives

Country Status (20)

Country Link
US (1) US9079922B2 (en)
EP (1) EP2776431B1 (en)
JP (1) JP6030146B2 (en)
KR (1) KR20140096337A (en)
AR (1) AR088691A1 (en)
AU (1) AU2012335207B2 (en)
BR (1) BR112014011064A8 (en)
CA (1) CA2854264A1 (en)
CL (1) CL2014001154A1 (en)
ES (1) ES2581056T3 (en)
HK (1) HK1202288A1 (en)
IL (1) IL232463A0 (en)
IN (1) IN2014CN04126A (en)
MX (1) MX344529B (en)
PL (1) PL2776431T3 (en)
RU (1) RU2616609C2 (en)
SG (1) SG11201401710PA (en)
TW (1) TWI594996B (en)
WO (1) WO2013068948A1 (en)
ZA (1) ZA201404176B (en)

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MA38588B1 (en) 2013-04-16 2018-04-30 Idorsia Pharmaceuticals Ltd Bi-aromatic antibacterial derivatives
AR096135A1 (en) 2013-05-02 2015-12-09 Actelion Pharmaceuticals Ltd DERIVATIVES OF QUINOLONA
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GB201602235D0 (en) * 2016-02-08 2016-03-23 Redx Pharma Plc Antibacterial compounds
WO2017137743A1 (en) * 2016-02-08 2017-08-17 Redx Pharma Plc Antibacterial compounds
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JP7148991B2 (en) * 2017-06-08 2022-10-06 バグワークス・リサーチ・インコーポレイテッド Heterocyclic compound useful as an antibacterial agent and method for producing the same
ES2952989T3 (en) * 2017-11-29 2023-11-07 Bugworks Res Inc Antibacterial heterocyclic compounds and their synthesis

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Also Published As

Publication number Publication date
TW201326166A (en) 2013-07-01
TWI594996B (en) 2017-08-11
SG11201401710PA (en) 2014-09-26
JP6030146B2 (en) 2016-11-24
RU2014123109A (en) 2015-12-20
JP2014532754A (en) 2014-12-08
EP2776431B1 (en) 2016-05-04
CA2854264A1 (en) 2013-05-16
AU2012335207B2 (en) 2017-05-25
CL2014001154A1 (en) 2014-09-12
KR20140096337A (en) 2014-08-05
ZA201404176B (en) 2016-05-25
HK1202288A1 (en) 2015-09-25
AR088691A1 (en) 2014-06-25
IL232463A0 (en) 2014-06-30
AU2012335207A1 (en) 2014-07-03
RU2616609C2 (en) 2017-04-18
PL2776431T3 (en) 2016-11-30
BR112014011064A2 (en) 2017-06-13
MX344529B (en) 2016-12-19
CN103917539A (en) 2014-07-09
WO2013068948A1 (en) 2013-05-16
US9079922B2 (en) 2015-07-14
US20150051188A1 (en) 2015-02-19
MX2014005637A (en) 2014-06-23
ES2581056T3 (en) 2016-08-31
EP2776431A1 (en) 2014-09-17
IN2014CN04126A (en) 2015-07-10

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B25A Requested transfer of rights approved

Owner name: IDORSIA PHARMACEUTICALS LTD (CH)

B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B25L Entry of change of name and/or headquarter and transfer of application, patent and certificate of addition of invention: publication cancelled

Owner name: ACTELION PHARMACEUTICALS LTD (CH)

B25C Requirement related to requested transfer of rights

Owner name: ACTELION PHARMACEUTICALS LTD (CH)

B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B25A Requested transfer of rights approved

Owner name: IDORSIA PHARMACEUTICALS LTD (CH)

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06T Formal requirements before examination [chapter 6.20 patent gazette]
B11E Dismissal acc. art. 34 of ipl - requirements for examination incomplete
B11T Dismissal of application maintained [chapter 11.20 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]